PROPERTIES, MODE OF ACTION AND EFFECTS OF ANTICANCER DRUGS

• Anticancer drugs


  Antineoplastic drugs used to treat malignancies or cancerous growths to control the growth of cancerous cells
• Major classes of anticancer drugs

  • Alkylating agents
  • Antimetabolites
  • Natural products
  • Hormones
• Chemotherapy more properly relates to the use of chemicals to treat disease in general, but it is often associated with the use of anticancer medications
• 1. fluorouracil (5-FU)


  An antimetabolite drug that is widely used for the treatment of cancer, particularly for colorectal cancer
• Mechanism of action of 5-FU

  1. Inhibition of thymidylate synthase (TS)

  2. Incorporation of its metabolites into RNA and DNA
• Modulation strategies for 5-FU

  Co-treatment with leucovorin and methotrexate to increase anticancer activity
• Molecular biomarkers for 5-FU

  mRNA and protein expression levels of TS
• DNA microarray analysis of 5-FU-responsive genes will greatly facilitate the identification of new biomarkers, novel therapeutic targets and the development of rational drug combinations
• 1. FU

  Affects RNA metabolism, the mechanism of anticancer medications
• Interference with cell division

  1. Targets the cell cycle

  2. Inhibits enzymes critical for cell division

  3. Halts cell proliferation, particularly of cancer cells
• DNA damage


  1. Activates repair mechanisms

  2. If damage is extensive, leads to programmed cell death (apoptosis)

  3. Unrepaired damage can lead to genomic instability and potentially cancerous growth
• Inhibition of signal transduction

  1. Targets specific molecules or receptors involved in signaling pathways

  2. Prevents aberrant signaling and halts tumor growth
• Immune system activation


  1. Overcomes cancer cell evasion strategies

  2. Activates the immune system to recognize and attack cancer cells

  3. Can be achieved through immune checkpoint inhibitors or therapies that enhance the immune response
• Hormonal modulation


  1. Manipulates hormone levels or interferes with hormone receptors

  2. Inhibits tumor growth through hormone therapy
• Angiogenesis inhibition


  1. Blocks vascular endothelial growth factor (VEGF)

  2. Prevents tumors from accessing nutrients and oxygen

  3. Leads to tumor shrinkage and inhibits metastasis
• 5% of cancer patients experience infections
• 99% of cases involve the effects of anticancer drugs
• 25% of cases involve the effects of anticancer drugs
• Cancer remains one of the most significant health challenges worldwide, affecting millions of individuals and families every year
• Anticancer medicines


  Also known as anticancer drugs, carcinogenic medicine or chemotherapeutic agents, play a crucial role in the treatment and management of various types of cancer
• Anticancer drugs


  Also known as antineoplastic drugs, are medications that are effective in the treatment of malignant, or cancerous, diseases
• Anticancer drugs


  • They target cells that have undergone genetic changes and are dividing at a fast and uncontrolled rate
  • They can target various aspects of cancer cell biology, including their ability to divide uncontrollably, evade cell death mechanisms, and spread to other parts of the body (metastasis)
• Anticancer drugs act through many different ways
• Properties of anticancer medicine


  The distinctive characteristics or attributes that define how these medications function, interact with the body, and exert their therapeutic effects in the treatment of cancer
• Properties of anticancer medicine

  • Molecular structure
  • Mechanism of action
  • Pharmacokinetics
  • Formulation
  • Target specificity
  • Potential side effects
• Target Specificity


  • Anticancer drugs are often designed to target specific molecular pathways or processes involved in cancer growth and progression, helping minimize damage to healthy cells while effectively targeting cancer cells
• Cytotoxicity


  • Many anticancer drugs exert their effects by inducing cytotoxicity, which refers to their ability to kill cancer cells
• Pharmacokinetics


  • Understanding the pharmacokinetics of anticancer medicines is crucial for optimizing their efficacy and minimizing adverse effects, including factors such as absorption, distribution, metabolism, and excretion of the drug within the body
• Mechanism of Action


  • Anticancer drugs can have diverse mechanisms of action, targeting different aspects of cancer cell biology. Some drugs inhibit enzymes or signaling pathways essential for cancer cell proliferation, while others interfere with DNA synthesis or repair mechanisms
• Chemical Structure


  • The chemical structure of anticancer medicines can vary widely, including small molecules, peptides, antibodies, and nucleic acid-based therapies leading to their unique properties and mechanisms of action
• Formulation


  • Anticancer drugs may be formulated in various dosage forms, including tablets, capsules, injections, or intravenous infusions, which can affect factors such as drug stability, bioavailability, and ease of administration
• Resistance


  • Cancer cells can develop resistance to anticancer drugs over time, limiting their effectiveness. Overcoming mechanisms of drug resistance is a critical aspect of cancer treatment
• Side Effects


  • Despite their benefits, anticancer medicines can also cause significant side effects due to their cytotoxic effects on healthy cells and tissues, including nausea, vomiting, hair loss, and immunosuppression
• The properties of anticancer medicines play a crucial role in their efficacy, safety, and clinical utility in the treatment and management of cancer. Understanding these properties is essential for optimizing treatment strategies and improving outcomes for cancer patients
• Classification of anticancer drugs

  The categorization of these medications based on various criteria such as their mechanism of action, chemical structure, therapeutic targets, or clinical indications
• Types of anticancer drugs


  Specific categories or classes of medications used in the treatment of cancer, encompassing a range of drug classes with distinct mechanisms of action and therapeutic properties, such as chemotherapeutic agents, targeted therapies, immunotherapies, hormonal therapies, and supportive medications
• Criteria for classifying anticancer drugs

  • Mechanism of action
  • Origin
• Growth Inhibitors (Angiogenesis Inhibition)


  • Tumor growth and metastasis depend on the formation of new blood vessels (angiogenesis) to supply nutrients and oxygen to cancer cells. Some anticancer drugs target angiogenesis pathways, inhibiting the growth of new blood vessels and depriving tumors of essential resources
• Division Inhibitors (Cell Cycle Disruption)

  • Cancer cells often exhibit dysregulated cell cycle control, leading to uncontrolled proliferation. Anticancer drugs may target components of the cell cycle machinery, such as cyclin-dependent kinases (CDKs), to disrupt cell cycle progression and induce cell death
• Direct Attack (DNA Damage)


  • Some anticancer drugs directly target and damage the DNA of cancer cells, interfering with their ability to replicate and survive